The present invention relates to new steroidal compounds which have valuable pharmacological properties.
For the treatment of certain forms of hypertonia, of edemas, of primary aldosteronism, and of other endocrinological imbalances caused by aldosterone, and for use as diuretics, compounds are employed which reverse the effect of aldosterone or deoxycorticosterone on the excretion of sodium and potassium salts. These include as their most well-known representative the compound spironolactone, which has been available commercially for some time. However, undesirable endocrinic side effects frequently occur in the treatment with spironolactone. These are evoked by the antiandrogenic and progestational activity of spironolactone. Thus, with a relatively long-term treatment of male patients with spironolactone, occurrence of gynecomastia is observed (Smith, W. G., The Lancet, 1962, p. 886; Mann, N. M., JAMA 1963, p. 778; Clark, E., JAMA 1965, p. 157; Greenblatt, D. J., JAMA 1973, p. 82) and impotence is observed as well (Greenblatt, D. J., JAMA 1973, p. 82), due to the antiandrogenic side effect of this active agent (Steelman, S. L. et al., Steroids 1963, p. 449; Schane, H. P., J. of Clinical Endocrinology and metabolism 1978, p. 691).
In contrast, the progestational side effects of spironolactone are blamed for secondary symptoms such as amenorrhea and cycle irregularities, in women treated with spironolactone. Both side effects can be confirmed in animal experiments as well as in vitro by the receptor binding test with the androgen and progestogen receptor, respectively.